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Items: 49


Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy.

Wardell SE, Yllanes AP, Chao CA, Bae Y, Andreano KJ, Desautels TK, Heetderks KA, Blitzer JT, Norris JD, McDonnell DP.

Breast Cancer Res Treat. 2019 Sep 27. doi: 10.1007/s10549-019-05454-y. [Epub ahead of print]


Targeting mutant estrogen receptors.

Wardell SE, Norris JD, McDonnell DP.

Elife. 2019 Jan 16;8. pii: e44181. doi: 10.7554/eLife.44181.


HOXB13 interaction with MEIS1 modifies proliferation and gene expression in prostate cancer.

Johng D, Torga G, Ewing CM, Jin K, Norris JD, McDonnell DP, Isaacs WB.

Prostate. 2019 Mar;79(4):414-424. doi: 10.1002/pros.23747. Epub 2018 Dec 17.


Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.

Tria GS, Abrams T, Baird J, Burks HE, Firestone B, Gaither LA, Hamann LG, He G, Kirby CA, Kim S, Lombardo F, Macchi KJ, McDonnell DP, Mishina Y, Norris JD, Nunez J, Springer C, Sun Y, Thomsen NM, Wang C, Wang J, Yu B, Tiong-Yip CL, Peukert S.

J Med Chem. 2018 Apr 12;61(7):2837-2864. doi: 10.1021/acs.jmedchem.7b01682. Epub 2018 Mar 22.


Neomorphic ERα Mutations Drive Progression in Breast Cancer and Present a Challenge for New Drug Discovery.

McDonnell DP, Norris JD, Chang CY.

Cancer Cell. 2018 Feb 12;33(2):153-155. doi: 10.1016/j.ccell.2018.01.014.


Androgen receptor antagonism drives cytochrome P450 17A1 inhibitor efficacy in prostate cancer.

Norris JD, Ellison SJ, Baker JG, Stagg DB, Wardell SE, Park S, Alley HM, Baldi RM, Yllanes A, Andreano KJ, Stice JP, Lawrence SA, Eisner JR, Price DK, Moore WR, Figg WD, McDonnell DP.

J Clin Invest. 2017 Jun 1;127(6):2326-2338. doi: 10.1172/JCI87328. Epub 2017 May 2.


Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.

Burks HE, Abrams T, Kirby CA, Baird J, Fekete A, Hamann LG, Kim S, Lombardo F, Loo A, Lubicka D, Macchi K, McDonnell DP, Mishina Y, Norris JD, Nunez J, Saran C, Sun Y, Thomsen NM, Wang C, Wang J, Peukert S.

J Med Chem. 2017 Apr 13;60(7):2790-2818. doi: 10.1021/acs.jmedchem.6b01468. Epub 2017 Mar 15.


CDK4/6 Therapeutic Intervention and Viable Alternative to Taxanes in CRPC.

Stice JP, Wardell SE, Norris JD, Yllanes AP, Alley HM, Haney VO, White HS, Safi R, Winter PS, Cocce KJ, Kishton RJ, Lawrence SA, Strum JC, McDonnell DP.

Mol Cancer Res. 2017 Jun;15(6):660-669. doi: 10.1158/1541-7786.MCR-17-0028. Epub 2017 Feb 16.


MMTV-PyMT and Derived Met-1 Mouse Mammary Tumor Cells as Models for Studying the Role of the Androgen Receptor in Triple-Negative Breast Cancer Progression.

Christenson JL, Butterfield KT, Spoelstra NS, Norris JD, Josan JS, Pollock JA, McDonnell DP, Katzenellenbogen BS, Katzenellenbogen JA, Richer JK.

Horm Cancer. 2017 Apr;8(2):69-77. doi: 10.1007/s12672-017-0285-6. Epub 2017 Feb 13.


Inhibiting androgen receptor nuclear entry in castration-resistant prostate cancer.

Pollock JA, Wardell SE, Parent AA, Stagg DB, Ellison SJ, Alley HM, Chao CA, Lawrence SA, Stice JP, Spasojevic I, Baker JG, Kim SH, McDonnell DP, Katzenellenbogen JA, Norris JD.

Nat Chem Biol. 2016 Oct;12(10):795-801. doi: 10.1038/nchembio.2131. Epub 2016 Aug 8.


Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging.

Gustafson JL, Neklesa TK, Cox CS, Roth AG, Buckley DL, Tae HS, Sundberg TB, Stagg DB, Hines J, McDonnell DP, Norris JD, Crews CM.

Angew Chem Int Ed Engl. 2015 Aug 10;54(33):9659-62. doi: 10.1002/anie.201503720. Epub 2015 Jun 17.


Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer.

McDonnell DP, Wardell SE, Norris JD.

J Med Chem. 2015 Jun 25;58(12):4883-7. doi: 10.1021/acs.jmedchem.5b00760. Epub 2015 Jun 3.


Efficacy of SERD/SERM Hybrid-CDK4/6 Inhibitor Combinations in Models of Endocrine Therapy-Resistant Breast Cancer.

Wardell SE, Ellis MJ, Alley HM, Eisele K, VanArsdale T, Dann SG, Arndt KT, Primeau T, Griffin E, Shao J, Crowder R, Lai JP, Norris JD, McDonnell DP, Li S.

Clin Cancer Res. 2015 Nov 15;21(22):5121-5130. doi: 10.1158/1078-0432.CCR-15-0360. Epub 2015 May 19.


Obesity, cholesterol metabolism, and breast cancer pathogenesis.

McDonnell DP, Park S, Goulet MT, Jasper J, Wardell SE, Chang CY, Norris JD, Guyton JR, Nelson ER.

Cancer Res. 2014 Sep 15;74(18):4976-82. doi: 10.1158/0008-5472.CAN-14-1756. Epub 2014 Jul 24.


Effects of repeated transvaginal aspiration of immature follicles on mare health and ovarian status.

Velez IC, Arnold C, Jacobson CC, Norris JD, Choi YH, Edwards JF, Hayden SS, Hinrichs K.

Equine Vet J Suppl. 2012 Dec;(43):78-83.


ELF3 is a repressor of androgen receptor action in prostate cancer cells.

Shatnawi A, Norris JD, Chaveroux C, Jasper JS, Sherk AB, McDonnell DP, Giguère V.

Oncogene. 2014 Feb 13;33(7):862-71. doi: 10.1038/onc.2013.15. Epub 2013 Feb 25.


A viable foal obtained by equine somatic cell nuclear transfer using oocytes recovered from immature follicles of live mares.

Choi YH, Norris JD, Velez IC, Jacobson CC, Hartman DL, Hinrichs K.

Theriogenology. 2013 Mar 15;79(5):791-6.e1. doi: 10.1016/j.theriogenology.2012.12.005. Epub 2013 Jan 11.


Evaluation of foal production following intracytoplasmic sperm injection and blastocyst culture of oocytes from ovaries collected immediately before euthanasia or after death of mares under field conditions.

Hinrichs K, Choi YH, Norris JD, Love LB, Bedford-Guaus SJ, Hartman DL, Velez IC.

J Am Vet Med Assoc. 2012 Oct 15;241(8):1070-4. doi: 10.2460/javma.241.8.1070.


The homeodomain protein HOXB13 regulates the cellular response to androgens.

Norris JD, Chang CY, Wittmann BM, Kunder RS, Cui H, Fan D, Joseph JD, McDonnell DP.

Mol Cell. 2009 Nov 13;36(3):405-16. doi: 10.1016/j.molcel.2009.10.020.


Inhibition of prostate cancer cell growth by second-site androgen receptor antagonists.

Joseph JD, Wittmann BM, Dwyer MA, Cui H, Dye DA, McDonnell DP, Norris JD.

Proc Natl Acad Sci U S A. 2009 Jul 21;106(29):12178-83. doi: 10.1073/pnas.0900185106. Epub 2009 Jul 2.


Induction of Kruppel-like factor 5 expression by androgens results in increased CXCR4-dependent migration of prostate cancer cells in vitro.

Frigo DE, Sherk AB, Wittmann BM, Norris JD, Wang Q, Joseph JD, Toner AP, Brown M, McDonnell DP.

Mol Endocrinol. 2009 Sep;23(9):1385-96. doi: 10.1210/me.2009-0010. Epub 2009 May 21.


Differential presentation of protein interaction surfaces on the androgen receptor defines the pharmacological actions of bound ligands.

Norris JD, Joseph JD, Sherk AB, Juzumiene D, Turnbull PS, Rafferty SW, Cui H, Anderson E, Fan D, Dye DA, Deng X, Kazmin D, Chang CY, Willson TM, McDonnell DP.

Chem Biol. 2009 Apr 24;16(4):452-60. doi: 10.1016/j.chembiol.2009.01.016.


Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic.

Sherk AB, Frigo DE, Schnackenberg CG, Bray JD, Laping NJ, Trizna W, Hammond M, Patterson JR, Thompson SK, Kazmin D, Norris JD, McDonnell DP.

Cancer Res. 2008 Sep 15;68(18):7475-83. doi: 10.1158/0008-5472.CAN-08-1047.


Single-step purification of full-length human androgen receptor.

Juzumiene D, Chang CY, Fan D, Hartney T, Norris JD, McDonnell DP.

Nucl Recept Signal. 2005;3:e001. Epub 2005 Oct 21.


Linking ligand-induced alterations in androgen receptor structure to differential gene expression: a first step in the rational design of selective androgen receptor modulators.

Kazmin D, Prytkova T, Cook CE, Wolfinger R, Chu TM, Beratan D, Norris JD, Chang CY, McDonnell DP.

Mol Endocrinol. 2006 Jun;20(6):1201-17. Epub 2006 Mar 30.


Structural basis for an unexpected mode of SERM-mediated ER antagonism.

Wu YL, Yang X, Ren Z, McDonnell DP, Norris JD, Willson TM, Greene GL.

Mol Cell. 2005 May 13;18(4):413-24.


Application of random peptide phage display to the study of nuclear hormone receptors.

Chang CY, Norris JD, Jansen M, Huang HJ, McDonnell DP.

Methods Enzymol. 2003;364:118-42. No abstract available.


Elucidation of the molecular mechanism of action of selective estrogen receptor modulators.

McDonnell DP, Wijayaratne A, Chang CY, Norris JD.

Am J Cardiol. 2002 Jul 3;90(1A):35F-43F. Review.


Connections and regulation of the human estrogen receptor.

McDonnell DP, Norris JD.

Science. 2002 May 31;296(5573):1642-4. Review.


Definition of the molecular and cellular mechanisms underlying the tissue-selective agonist/antagonist activities of selective estrogen receptor modulators.

McDonnell DP, Connor CE, Wijayaratne A, Chang CY, Norris JD.

Recent Prog Horm Res. 2002;57:295-316. Review.


A negative coregulator for the human ER.

Norris JD, Fan D, Sherk A, McDonnell DP.

Mol Endocrinol. 2002 Mar;16(3):459-68.


Capitalizing on the complexities of estrogen receptor pharmacology in the quest for the perfect SERM.

McDonnell DP, Chang CY, Norris JD.

Ann N Y Acad Sci. 2001 Dec;949:16-35.


Estrogen receptor-cofactor interactions as targets for novel drug discovery.

Norris JD, Chang C, McDonnell DP.

Ernst Schering Res Found Workshop. 2001;(34):181-201. Review. No abstract available.


Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational changes in the estrogen receptor.

Connor CE, Norris JD, Broadwater G, Willson TM, Gottardis MM, Dewhirst MW, McDonnell DP.

Cancer Res. 2001 Apr 1;61(7):2917-22.


Development of peptide antagonists that target estrogen receptor-cofactor interactions.

McDonnell DP, Chang CY, Norris JD.

J Steroid Biochem Mol Biol. 2000 Nov 30;74(5):327-35. Review.


Modulation of estrogen receptor-alpha transcriptional activity by the coactivator PGC-1.

Tcherepanova I, Puigserver P, Norris JD, Spiegelman BM, McDonnell DP.

J Biol Chem. 2000 May 26;275(21):16302-8.


Comparative analyses of mechanistic differences among antiestrogens.

Wijayaratne AL, Nagel SC, Paige LA, Christensen DJ, Norris JD, Fowlkes DM, McDonnell DP.

Endocrinology. 1999 Dec;140(12):5828-40.


Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors alpha and beta.

Chang Cy, Norris JD, Grøn H, Paige LA, Hamilton PT, Kenan DJ, Fowlkes D, McDonnell DP.

Mol Cell Biol. 1999 Dec;19(12):8226-39.


Peptide antagonists of the human estrogen receptor.

Norris JD, Paige LA, Christensen DJ, Chang CY, Huacani MR, Fan D, Hamilton PT, Fowlkes DM, McDonnell DP.

Science. 1999 Jul 30;285(5428):744-6.


Estrogen receptor (ER) modulators each induce distinct conformational changes in ER alpha and ER beta.

Paige LA, Christensen DJ, Grøn H, Norris JD, Gottlin EB, Padilla KM, Chang CY, Ballas LM, Hamilton PT, McDonnell DP, Fowlkes DM.

Proc Natl Acad Sci U S A. 1999 Mar 30;96(7):3999-4004.


Dissection of the molecular mechanism of action of GW5638, a novel estrogen receptor ligand, provides insights into the role of estrogen receptor in bone.

Willson TM, Norris JD, Wagner BL, Asplin I, Baer P, Brown HR, Jones SA, Henke B, Sauls H, Wolfe S, Morris DC, McDonnell DP.

Endocrinology. 1997 Sep;138(9):3901-11.


Identification of a third autonomous activation domain within the human estrogen receptor.

Norris JD, Fan D, Kerner SA, McDonnell DP.

Mol Endocrinol. 1997 Jun;11(6):747-54.


Estrogenic activity of a dieldrin/toxaphene mixture in the mouse uterus, MCF-7 human breast cancer cells, and yeast-based estrogen receptor assays: no apparent synergism.

Ramamoorthy K, Wang F, Chen IC, Norris JD, McDonnell DP, Leonard LS, Gaido KW, Bocchinfuso WP, Korach KS, Safe S.

Endocrinology. 1997 Apr;138(4):1520-7.


Potency of combined estrogenic pesticides.

Ramamoorthy K, Wang F, Chen IC, Safe S, Norris JD, McDonnell DP, Gaido KW, Bocchinfuso WP, Korach KS.

Science. 1997 Jan 17;275(5298):405-6. No abstract available.


Benzene hexachloride poisoning in cattle.

Ray AC, Norris JD, Reagor JC.

J Am Vet Med Assoc. 1975 Jun 15;166(12):1180-2.


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